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]quinoline derivatives were synthesized and evaluated
for their anticancer activities against human cervical epithelioid carcinoma
(HeLa), hepatocelluar carcinoma (SKHep1), oral squamous cell carcinoma (SAS),
human stomach adenocarcinoma (AGS), non-small cell lung cancer (A549), and
esophageal carcinoma (CE81T). Among these compounds tested, 1-[4-(furo[2,3-
) was the most potent with
values of less than 4.2 micromole respectively against the growth of HeLa, SKHep, and
CE81T cells and therefore, was further evaluated on its eff
ects of cell cycle distribution.
Results indicated that lead compound
induces cell cycle arrest in G2/M followed by
apoptosis. However, some drawbacks such as lack of selective cytotoxicity, poor oral
bioavailability, and poor water solubility exhibited by
prompted us to search for
newer derivatives with better pharmacokinetic profi
les and higher water solubility.
Various aminoalkoxyimino derivatives of
have been synthesized and evaluated.
Some of them exhibited selective anticancer activity against the growth of non-small
cell lung cancers (especially NCI-H460) and higher water solubility than the lead
compound. Xenograghic studies and orthotropic lung cancer model in nude mice
using H1229 cells indicated that certain aminoalkoxyimino derivatives of
cacy in inhibiting tumor growth
. Further structural optimization
and mechanism studies are on-going.
Dr. Cherng-Chyi Tzeng has completed his Ph. D degree from the University of Rhode Island,
USA in 1984. He is the Dean of General Affairs at Kaohsiung Medical University, Taiwan. He
has published more than 120 papers in reputed journals and serving as an editorial board
Kaohsiung Journal of Medical Sciences
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